Targeting Transcriptional Enhanced Associate Domains (TEADs) - PubMed (original) (raw)

Review

. 2018 Jun 28;61(12):5057-5072.

doi: 10.1021/acs.jmedchem.7b00879. Epub 2017 Dec 28.

Affiliations

• PMID: 29251924
• DOI: 10.1021/acs.jmedchem.7b00879

Review

Targeting Transcriptional Enhanced Associate Domains (TEADs)

Floriane Gibault et al. J Med Chem. 2018.

Abstract

Transcriptional enhanced associate domain (TEAD) proteins are the downstream effectors of the Hippo signaling pathway that regulate cell proliferation and stem cell functions. TEADs are unable to activate transcription and require the help of coactivators such as YAP, TAZ, VgLL, and p160 proteins. The expression of TEAD family is up-regulated in many cancer types including gastric, colorectal, breast, and prostate cancers, which is correlated with poor survival in patients. Pharmacological modulators of TEADs could therefore find application in cancer treatment and regenerative medicine. In this review, we present the very recent available structures of TEADs with or without coactivators or inhibitors and discuss the potential therapeutic application of their ligands.

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